MRP

PACKING

GLIMEPIRIDE

Glimepiride is a sulfonylurea which works by increasing the amount of insulin released by the pancreas in order to lower the blood glucose.

METFORMIN

Metformin is a biguanide which works by lowering glucose production in the liver, delaying glucose absorption from intestines and increasing the body’s sensitivity to insulin.

GLIMEPIRIDE

Glimepiride is a sulphonylurea antihyperglycemic agent that may be given in a single daily dose. It acts by stimulating insulin release from pancreatic beta-cells and possibly also via extrapancreatic mechanisms. The major site of activity of Glimepiride is thought to be membrane receptors on pancreatic beta-cells, where it acts via ATP-regulated potassium (KATP) channels, resulting in membrane depolarisation and release of insulin. Glimepiride is also internalised into pancreatic beta-cells, where it associates with secretory granules. This internalisation is thought to reflect insulinotropic mechanisms of Glimepiride other than at potassium channels. Glimepiride decreases blood glucose and increases blood insulin levels, with maximum effects during the first 4 hours after the dose.

METFORMIN

Metformin is a biguanide with antihyperglycemic effects, lowering both basal and postprandial plasma glucose. It does not stimulate insulin secretion and therefore does not produce hypoglycemia.

Pharmacokinetics

GLIMEPIRIDE:

Absorption:

Bioavailability is 100%. Cmax is about 103 to 591 ng/mL (dose dependent). T max is about 2 to 3 h.

Distribution:

Vd is 8.8 L. Protein binding is more than 99.5%.

Metabolism:

Completely metabolized by oxidation via CYP-450 2C9. Major metabolites are cyclohexylhydroxymethyl (M1) (about one-third of the activity of the parent) and carboxyl (M2) derivatives.

Excretion:

About 60% is excreted in urine and about 40% in feces as metabolites. The half-life is about 5 to 9.2 h.

METFORMIN:

Absorption:

After an oral dose of metformin, time to peak plasma concentration (Tmax) is reached in 2.5 hours. Absolute bioavailability of a 500 mg metformin tablet is approximately 50% to 60% in healthy subjects. Food decreases the extent of absorption and slightly delays absorption.

Distribution:

Plasma protein binding is negligible. Metformin partitions into erythrocytes. The blood peak is lower than the plasma peak and appears approximately the same time. The red blood cells most likely represent a secondary compartment of distribution. The mean Vd ranges between 63 to 276 L.

Metabolism:

Metformin is excreted unchanged in urine. No metabolites have been identified in humans.

Elimination:

Renal clearance of metformin is >400 ml/min, indicating that metformin is eliminated by glomerular filtration and tubular secretion. Following an oral dose, the apparent terminal elimination half-life is approximately 6.5 hours. When renal function is impaired, renal clearance is decreased in proportion to that of creatinine and thus the elimination half-life is prolonged, leading to increased levels of metformin in plasma.

ABOUT US

Trumac Healthcare is a leading PCD pharma company in India. We are manufacturers and suppliers of finished pharma medicines since last 10 years all over India. We have a wide range of product portfolio consisting of tablets, capsules, injectable, syrups, ointments, eye, ear and nasal drops & Ayurvedic Medicines. Our products are manufactured at one of the best state of art manufacturing facilities, which are WHO and GMP certified units.